It is recalled that fenofibrate is isopropyl para-(4-chlorobenzoyl)-pehnoxyisobutyrate. In the present application, the term "fenofibrate and its derivatives" is used to designate compounds having formula I: ##STR1## in which:
R.sub.1 represents a phenyl group or a phenyl group substituted by one or more --CH.sub.3, CF.sub.3 or by halogens (in particular fluorine, chlorine, or bromine);
R.sub.2 and R.sub.3 independently represent a hydrogen atom or a halogen atom (preferably fluorine, chlorine, or bromine), an alkyl or an alkoxy group having 1 to 5 C or one of the following groups: --CF.sub.3, --SCH.sub.3, --SOCH.sub.3, --SO.sub.2 CH.sub.3, or --OH; and
Y represents one of the following groups: --OH; inferior alkoxy, preferably in C.sub.1 -C.sub.4 ; --NR.sub.4 R.sub.5 ; --NHCH.sub.2 CH.sub.2 NR.sub.4 R.sub.5 ; or --O--alkylene--NR.sub.4 R.sub.5, with the alkylene having, in particular, two to six atoms of carbon, and with R.sub.4 and R.sub.5 being identical or different and each representing a hydrogen atom or one of the following groups: C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 and preferably C.sub.5 -C.sub.6 cycloalkyl; aryl or aryl substituted on the aromatic residue by one or more halogen, methyl, or --CF.sub.3 groups; or else R.sub.4 and R.sub.5 constitute, together with the nitrogen atom to which they are connected, one of the following groups: either an n-heterocyclic group having 5 to 7 vertices capable of enclosing a second hetero-atom selected from N, O, and S, and capable of being substituted; or else an amide residue derived from lysine or cysteine.
Naturally, the expression "fenofibrate and its derivatives" also covers the salts that can be obtained from compounds of formula I by adding pharmaceutically acceptable acids.
Fenofibrate is used in the treatment of adult endogenous hyperlipidaemia, hypercholesterolaemia, and hypertrigylceridaemia. Thus, in an adult being treated with 300 to 400 mg per day of fenofibrate, there can be observed a 20% to 25% reduction in cholesterolaemia and a 40% to 50% reduction in triglyceridaemia.
The unaltered substance is not found in plasma. The major plasmatic metabolite is fenofibric acid.
On average, the maximum concentration in plasma is reached five hours after taking the medicine. The average concentration in plasma is about 50 micrograms/ml for a dose of 300 mg of fenofibrate per day. This level is stable throughout continuous treatment.
Fenofibric acid is strongly bound to plasmatic albumin and can displace antivitamins K from protein fixing sites and potentialize their anticoagulant effect.
The half-life for eliminating fenofibric acid from plasma is about twenty hours.
Under these conditions, it will be understood that there is no need to take it more than once a day.
It has been observed that fenofibrate has poor solubility in aqueous liquids, thereby giving rise to non-uniform absorption in the digestive tube, and in accordance with the present invention a galenical preparation has been devised which considerably improves absorption by the digestive tube.